ES2305062T3 - Inhibidores basados en pirolidina condensados con ciclopropilo de la pipeptidil peptidasa iv, procedimientos para su preparacion, y su uso. - Google Patents
Inhibidores basados en pirolidina condensados con ciclopropilo de la pipeptidil peptidasa iv, procedimientos para su preparacion, y su uso. Download PDFInfo
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- ES2305062T3 ES2305062T3 ES01918383T ES01918383T ES2305062T3 ES 2305062 T3 ES2305062 T3 ES 2305062T3 ES 01918383 T ES01918383 T ES 01918383T ES 01918383 T ES01918383 T ES 01918383T ES 2305062 T3 ES2305062 T3 ES 2305062T3
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- 238000000034 method Methods 0.000 title claims description 110
- 239000003112 inhibitor Substances 0.000 title claims description 82
- 238000002360 preparation method Methods 0.000 title claims description 11
- 102000035195 Peptidases Human genes 0.000 title description 3
- 108091005804 Peptidases Proteins 0.000 title description 3
- 235000019833 protease Nutrition 0.000 title description 2
- XIPUIGPNIDKXJU-UHFFFAOYSA-N [CH]1CC1 Chemical class [CH]1CC1 XIPUIGPNIDKXJU-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 271
- -1 amino, substituted amino Chemical group 0.000 claims abstract description 95
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 47
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 38
- 125000003118 aryl group Chemical group 0.000 claims abstract description 35
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 23
- 125000003342 alkenyl group Chemical group 0.000 claims abstract description 22
- 125000003710 aryl alkyl group Chemical group 0.000 claims abstract description 22
- 125000000304 alkynyl group Chemical group 0.000 claims abstract description 21
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 19
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims abstract description 17
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract description 16
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims abstract description 16
- 125000005350 hydroxycycloalkyl group Chemical group 0.000 claims abstract description 16
- 125000005843 halogen group Chemical group 0.000 claims abstract description 14
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims abstract description 14
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims abstract description 13
- 125000004414 alkyl thio group Chemical group 0.000 claims abstract description 12
- 125000000392 cycloalkenyl group Chemical group 0.000 claims abstract description 12
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims abstract description 11
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims abstract description 10
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- 125000005842 heteroatom Chemical group 0.000 claims abstract description 10
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- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims abstract description 8
- 125000004949 alkyl amino carbonyl amino group Chemical group 0.000 claims abstract description 8
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims abstract description 8
- 239000001257 hydrogen Substances 0.000 claims abstract description 8
- 229910052717 sulfur Inorganic materials 0.000 claims abstract description 8
- 125000002252 acyl group Chemical group 0.000 claims abstract description 7
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims abstract description 6
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims abstract description 6
- 125000003282 alkyl amino group Chemical group 0.000 claims abstract description 5
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- 125000001769 aryl amino group Chemical group 0.000 claims abstract description 4
- 125000005162 aryl oxy carbonyl amino group Chemical group 0.000 claims abstract description 4
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- 125000006684 polyhaloalkyl group Polymers 0.000 claims abstract description 4
- 125000005089 alkenylaminocarbonyl group Chemical group 0.000 claims abstract description 3
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- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 7
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
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| US18855500P | 2000-03-10 | 2000-03-10 | |
| US188555P | 2000-03-10 | ||
| PCT/US2001/007151 WO2001068603A2 (en) | 2000-03-10 | 2001-03-05 | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use |
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| ES10178907.1T Expired - Lifetime ES2553573T3 (es) | 2000-03-10 | 2001-03-05 | Ácido (amino protegido)-hidroxi-adamantano-carboxílico y procedimiento para su preparación |
| ES01918383T Expired - Lifetime ES2305062T3 (es) | 2000-03-10 | 2001-03-05 | Inhibidores basados en pirolidina condensados con ciclopropilo de la pipeptidil peptidasa iv, procedimientos para su preparacion, y su uso. |
| ES15186007T Expired - Lifetime ES2768961T3 (es) | 2000-03-10 | 2001-03-05 | Inhibidores de dipeptidil peptidasa IV basados en pirrolidina condensada con ciclopropilo y su uso farmacéutico |
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| ES10178907.1T Expired - Lifetime ES2553573T3 (es) | 2000-03-10 | 2001-03-05 | Ácido (amino protegido)-hidroxi-adamantano-carboxílico y procedimiento para su preparación |
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